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1. 发明申请

US20090099250A1 BENZOCYCLOHEPTENE DERIVATIVES AS ESTROGENS HAVING SELECTIVE ACTIVITY 审中-公开
标题翻译：作为具有选择性活性的雌激素的苄基胆碱衍生物
公开(公告)号：US20090099250A1
公开(公告)日：2009-04-16
申请号：US12249056
申请日：2008-10-10
申请人： Ralf WYRWA , Olaf Peters , Rolf Bohlmann , Peter Droescher , Katja Prelle , Karl Heinrich Fritzemeier , Hans Peter Muhn
发明人： Ralf WYRWA , Olaf Peters , Rolf Bohlmann , Peter Droescher , Katja Prelle , Karl Heinrich Fritzemeier , Hans Peter Muhn
IPC分类号： A61K31/381 , C07C39/17 , A61K31/122 , A61K31/05 , A61P5/00 , C07C49/747 , C07D333/16
CPC分类号： C07C39/23 , C07C39/17 , C07C43/23 , C07D333/16
摘要： The present invention describes non-steroidal compounds of the general formula (I) in which A is in which X1 means one or more groups on the phenyl ring and represents independently of one another a halogen, OH, (C1-C4)alkyl, (C1-C4)alkyl-O, (C3-C6)cycloalkyl-O, (C1-C14)acyl-O, (C1-C4)alkenyl, (C1-C4)alkynyl, perfluoro(C1-C4)alkyl radical, —CHO or CN, and X2 means one or more groups on the phenyl ring and represents independently of one another an H, halogen, OH, (C1-C4)alkyl, (C1-C4)alkyl-O, (C1-C4)alkenyl, (C1-C4)alkynyl, perfluoro-(C1-C4)alkyl radical, —CHO or CN, as Estrogens.
摘要翻译：本发明描述了通式（I）的非甾体化合物，其中A是其中X 1表示苯基上的一个或多个基团并且彼此独立地表示卤素，OH，（C 1 -C 4）烷基，（ C1-C4）烷基-O，（C3-C6）环烷基-O，（C1-C14）酰基-O，（C1-C4）烯基，（C1-C4）炔基，全氟（C1-C4）烷基， CHO或CN，X2表示苯基上的一个或多个基团，并且彼此独立地表示H，卤素，OH，（C1-C4）烷基，（C1-C4）烷基-O，（C1-C4）烯基，（C 1 -C 4）炔基，全氟 - （C 1 -C 4）烷基，-CHO或CN作为雌激素。

2. 发明申请

US20070197488A1 Prodrugs of ERbeta-selective substances, process for their production, and pharmaceutical compositions that contain these compounds 审中-公开
标题翻译： ERbeta选择性物质的前体药物，其制备方法和含有这些化合物的药物组合物
公开(公告)号：US20070197488A1
公开(公告)日：2007-08-23
申请号：US11605472
申请日：2006-11-29
申请人： Olaf Peters , Gudrun Reddersen , Ralf Wyrwa , Alexander Hillisch , Walter Elger , Katja Prelle , Peter Droescher
发明人： Olaf Peters , Gudrun Reddersen , Ralf Wyrwa , Alexander Hillisch , Walter Elger , Katja Prelle , Peter Droescher
IPC分类号： A61K31/565
CPC分类号： C07J41/0044
摘要： This invention provides prodrugs of 8β-substituted estratrienes of general formula (I), in which the group Z is bonded to the steroid, process for their production, pharmaceutical compositions that contain these compounds as well as use thereof. The compounds of general formula I according to the invention do not bind to the estrogen receptor α and/or β. They bind to carbonic anhydrases and inhibit these enzymes.
摘要翻译：本发明提供通式（I）的8-取代的雌三烯的前药，其中基团Z与类固醇结合，其制备方法，含有这些化合物的药物组合物及其用途。根据本发明的通式I的化合物不与雌激素受体α和/或β结合。它们与碳酸酐酶结合并抑制这些酶。

3. 发明申请

US20090029957A1 8-BETA-SUBSTITUTED ESTRATRIENES AS SELECTIVELY ACTIVE ESTROGENS 审中-公开
标题翻译： 8-BETA取代的ESTRATRIENES作为选择性活动的ESTROGENS
公开(公告)号：US20090029957A1
公开(公告)日：2009-01-29
申请号：US12171424
申请日：2008-07-11
申请人： Olaf Peters , Nico Braeuer , Ina Thieme , Katja Prelle , Peter Muhn , Karl Heinrich Fritzemeier
发明人： Olaf Peters , Nico Braeuer , Ina Thieme , Katja Prelle , Peter Muhn , Karl Heinrich Fritzemeier
IPC分类号： A61K31/56 , A61K31/565 , C07J1/00 , A61P37/00 , A61P35/00 , A61P17/00 , A61P17/14 , A61P9/00 , A61P1/00
CPC分类号： C07J1/007 , C07J1/0062
摘要： The invention refers to 8β-substituted estra-1,3,5(10)-triene derivatives of general formula I their use as pharmaceutical active ingredients, which have in vitro a higher affinity to estrogen receptor preparations from rat prostates than to estrogen receptor preparations from rat uteri and in vivo a preferential action in the ovary in comparison to the uterus, their production, their therapeutic use and pharmaceutical dispensing forms that contain the new compounds.
摘要翻译：本发明涉及通式I的8-取代的雌-1,3,5（10） - 三烯衍生物，其用作药物活性成分，其具有比雌激素受体制剂在体外对雌激素受体制剂更高的亲和力与子宫相比，子宫中的子宫，其产生，其治疗用途和含有新化合物的药物分配形式相比在体内具有优先的作用。

4. 发明申请

US20050065135A1 8beta-Vinyl-11beta-(omega-substituted)alkyl-estra-1,3,5(10)-trienes 失效
标题翻译： 8beta-Vinyl-11beta-（ω-取代）烷基 - 雌-1,3,5（10） - 三烯
公开(公告)号：US20050065135A1
公开(公告)日：2005-03-24
申请号：US10829390
申请日：2004-04-22
申请人： Nico Braeuer , Olaf Peters , Alexander Hillisch , Rolf Bohlmann , Margit Richter , Hans-Peter Muhn
发明人： Nico Braeuer , Olaf Peters , Alexander Hillisch , Rolf Bohlmann , Margit Richter , Hans-Peter Muhn
IPC分类号： A61K31/56 , A61K31/565 , A61K31/566 , A61P15/16 , A61P15/18 , A61P35/00 , C07J20060101 , C07J1/00 , C07J5/00 , C07J7/00 , C07J75/00
CPC分类号： C07J5/00 , C07J7/00 , C07J75/00
摘要： This invention relates to 8β-vinyl-11β-(ω-substituted)alkyl-estra-1,3,5(10)-trienes of general formula I with ERβ-antagonistic activity, process for their production, their intermediate products, pharmaceutical preparations that contain the compounds according to the invention, as well as their use for the production of pharmaceutical agents. The new compounds can be used for contraception in men and women without influencing other estrogen-sensitive organs such as the uterus or the liver. They are also suitable for treating benign or malignant proliferative diseases of the ovary, such as ovarian cancer and granulosa cell tumors.
摘要翻译：本发明涉及具有ERβ-拮抗活性的通式I的8-乙烯基-11β-（ω-取代的）烷基 - 雌-1,3,5（10） - 三烯，其生产方法，其中间产物，药物制剂其含有根据本发明的化合物，以及它们用于生产药剂的用途。新化合物可用于男性和女性避孕，而不影响其他雌激素敏感性器官如子宫或肝脏。它们也适用于治疗卵巢的良性或恶性增殖性疾病，如卵巢癌和颗粒细胞瘤。

5. 发明授权

US07375098B2 8β-vinyl-11β-(ω-substituted)alkyl-estra-1,3,5(10)-trienes 失效
标题翻译： 8beta-vinyl-11beta-（ω-取代的）烷基 - 雌-1,3,5（10） - 三烯
公开(公告)号：US07375098B2
公开(公告)日：2008-05-20
申请号：US10829390
申请日：2004-04-22
申请人： Nico Braeuer , Olaf Peters , Alexander Hillisch , Rolf Bohlmann , Margit Richter , Hans-Peter Muhn
发明人： Nico Braeuer , Olaf Peters , Alexander Hillisch , Rolf Bohlmann , Margit Richter , Hans-Peter Muhn
IPC分类号： A61K31/56 , A61K31/58 , C07J1/00
CPC分类号： C07J5/00 , C07J7/00 , C07J75/00
摘要： This invention relates to 8β-vinyl-11β-(ω-substituted)alkyl-estra-1,3,5(10)-trienes of general formula I with ERβ-antagonistic activity, process for their production, their intermediate products, pharmaceutical preparations that contain the compounds according to the invention, as well as their use for the production of pharmaceutical agents. The new compounds can be used for contraception in men and women without influencing other estrogen-sensitive organs such as the uterus or the liver.They are also suitable for treating benign or malignant proliferative diseases of the ovary, such as ovarian cancer and granulosa cell tumors.
摘要翻译：本发明涉及具有ERβ-拮抗活性的通式I的8-乙烯基-11β-（ω-取代的）烷基 - 雌-1,3,5（10） - 三烯，其生产方法，其中间产物，药物制剂其含有根据本发明的化合物，以及它们用于生产药剂的用途。新化合物可用于男性和女性避孕，而不影响其他雌激素敏感性器官如子宫或肝脏。它们也适用于治疗卵巢的良性或恶性增殖性疾病，如卵巢癌和颗粒细胞瘤。

6. 发明申请

US20080182829A1 8Beta-Hydrocarbyl-Substituted Estratrienes As Selectively Active Estrogens 审中-公开
标题翻译： 8Beta-Hydrocarbyl-Substituted Estratrienes As Selective Active Estrogens
公开(公告)号：US20080182829A1
公开(公告)日：2008-07-31
申请号：US12045979
申请日：2008-03-11
申请人： Olaf Peters , Alexander Hillisch , Ina Thieme , Walter Elger , Christa Hegele-Hartung , Uwe Kollenkirchen , Karl-Heinrich Fritzemeier , Vladimir Patchev
发明人： Olaf Peters , Alexander Hillisch , Ina Thieme , Walter Elger , Christa Hegele-Hartung , Uwe Kollenkirchen , Karl-Heinrich Fritzemeier , Vladimir Patchev
IPC分类号： A61K31/58 , A61K31/565 , A61P25/28 , A61P19/02 , A61P1/00 , A61P15/00
CPC分类号： C07J1/007 , C07J1/0059 , C07J1/0062 , C07J1/0074 , C07J41/0072
摘要： This invention describes the new 8β-substituted estratrienes of general formula I in which R2, R3, R6, R6′, R7, R7′, R9, R11, R11′, R12, R14, R15, R15′, R16, R16′, R17, R17′ have the meanings that are indicated in the description, and R8 means a straight-chain or branched-chain, optionally partially or completely halogenated alkyl or alkenyl radical with up to 5 carbon atoms, an ethinyl- or prop-1-inyl radical, as pharmaceutical active ingredients that have in vitro a higher affinity to estrogen receptor preparations of rat prostates than to estrogen receptor preparations of rat uteri and in vivo preferably a preferential action on bone rather than the uterus and/or a pronounced action with respect to stimulation of the expression of 5HT2a-receptors and 5HT2a-transporters, their production, their therapeutic use and pharmaceutical dispensing forms that contain the new compounds. The invention also describes the use of these compounds for treatment of estrogen-deficiency-induced diseases and conditions as well as the use of an 8β-substituted estratriene structural part in the total structures of compounds that have a dissociation in favor of their estrogenic action on bones rather than the uterus.
摘要翻译：本发明描述了通式I的新的8-取代的雌三烯，其中R 2，R 3，R 6，R 6， R 7，R 7，R 9，R 11，R 11， > 11'，R 12，R 14，R 15，R 15'，R 15， R 16，R 16，R 17，R 17，R 17具有在说明书中指出的含义， R 8是指具有至多5个碳原子的直链或支链，任选部分或完全卤代的烷基或烯基，乙炔基或丙-1-基基团作为药物活性物质具有体外对大鼠前列腺的雌激素受体制剂的亲和力高于大鼠子宫雌激素受体制剂的体内成分，并且在体内优选对骨骼而不是子宫的优先作用和/或对刺激表达的显着作用 5HT2a受体和5HT2a转运蛋白，它们的产物 n，其治疗用途和含有新化合物的药物分配形式。本发明还描述了这些化合物用于治疗雌激素缺乏诱导的疾病和病症的用途，以及在具有有利于其雌激素作用的解离的化合物的总体结构中使用8-取代的雌三醇结构部分骨头而不是子宫。

7. 发明授权

US07378404B2 8β-hydrocarbyl-substituted estratrienes for use as selective estrogens 失效
标题翻译：用作选择性雌激素的8-烃基取代的雌三烯
公开(公告)号：US07378404B2
公开(公告)日：2008-05-27
申请号：US10257288
申请日：2001-04-12
申请人： Olaf Peters , Alexander Hillisch , Ina Thieme , Walter Elger , Christa Hegele-Hartung , Uwe Kollenkirchen , Karl-Heinrich Fritzemeier , Vladimir Patchev
发明人： Olaf Peters , Alexander Hillisch , Ina Thieme , Walter Elger , Christa Hegele-Hartung , Uwe Kollenkirchen , Karl-Heinrich Fritzemeier , Vladimir Patchev
IPC分类号： A61K31/56 , C07J1/00
CPC分类号： C07J1/007 , C07J1/0059 , C07J1/0062 , C07J1/0074 , C07J41/0072
摘要： This invention describes the new 8β-substituted estratrienes of general formula I in which R2, R3, R6, R6′, R7, R7′, R9, R11, R11′, R12, R14, R15, R15′, R16, R16′, R17 and R17′ have the meanings that are indicated in the description, and R8 means a straight-chain or branched-chain, optionally partially or completely halogenated alkyl or alkenyl radical with up to 5 carbon atoms, an ethinyl- or prop-1-inyl radical, as pharmaceutical active ingredients that have in vitro a higher affinity to estrogen receptor preparations of rat prostates than to estrogen receptor preparations of rat uteri and in vivo preferably a preferential action on bone rather than the uterus and/or a pronounced action with respect to stimulation of the expression of 5HT2a-receptors and 5HT2a-transporters, their production, their therapeutic use and pharmaceutical dispensing forms that contain the new compounds. The invention also describes the use of these compounds for treatment of estrogen-deficiency-induced diseases and conditions as well as the use of an 8β-substituted estratriene structural part in the total structures of compounds that have a dissociation in favor of their estrogenic action on bones rather than the uterus.
摘要翻译：本发明描述了通式I的新的8-取代的雌三烯，其中R 2，R 3，R 6，R 6， R 7，R 7，R 9，R 11，R 11， > 11'，R 12，R 14，R 15，R 15'，R 15， R 16，R 17，R 17和R 17'具有在说明书中指出的含义， R 8是指具有至多5个碳原子的直链或支链，任选部分或完全卤代的烷基或烯基，乙炔基或丙-1-基基团作为药物活性物质具有体外对大鼠前列腺的雌激素受体制剂的亲和力高于大鼠子宫雌激素受体制剂的体内成分，并且在体内优选对骨骼而不是子宫的优先作用和/或对刺激表达的显着作用 5HT2a受体和5HT2a转运蛋白，其产品其治疗用途和含有新化合物的药物分配形式。本发明还描述了这些化合物用于治疗雌激素缺乏诱导的疾病和病症的用途，以及在具有有利于其雌激素作用的解离的化合物的总体结构中使用8-取代的雌三醇结构部分骨头而不是子宫。

8. 发明申请

US20050148560A1 Prevention and treatment of hypertensive heart diseases by the selective estrogens 8beta-vinyl-estra-1,3,5(10)-trien-3,17beta-diol and 17beta-fluor-9alpha-vinyl-estra-1,3,5(10)-trien-3,16alpha-diol 审中-公开
标题翻译：通过选择性雌激素8beta-vinyl-estra-1,3,5（10） - 三烯-3,17β-二醇和17β-氟-9α-乙烯基 - 雌-1,3,5（ 10） - 三烯-3,16α-二醇
公开(公告)号：US20050148560A1
公开(公告)日：2005-07-07
申请号：US10995552
申请日：2004-11-24
申请人： Karl-Heinrich Fritzemeier , Christa Hegele-Hartung , Ludwig Neyses , Theo Pelzer , Olaf Peters
发明人： Karl-Heinrich Fritzemeier , Christa Hegele-Hartung , Ludwig Neyses , Theo Pelzer , Olaf Peters
IPC分类号： A61K31/565 , A61K31/56
CPC分类号： A61K31/565
摘要： The present invention relates to the use of the ERβ agonists 8β-Vinyl-estra-1,3,5(10)-trien-3,17β-diol and 17β-Fluor-9α-vinyl-estra-1,3,5(10)-trien-3,16α-diol for production of medicaments for the prevention and/or treatment of hypertensive heart disease, especially for the prevention and/or treatment of one or more of the conditions selected from the group of (1) hypertension, (2) cardiac hypertrophy and (3) heart failure.
摘要翻译：本发明涉及ERβ激动剂8beta-Vinyl-estra-1,3,5（10） - 三烯-3,17b-二醇和17β-Fluor-9α-乙烯基 - 雌-1,3,5（ 10） - 三烯-3βα-二醇用于生产用于预防和/或治疗高血压心脏病的药物，特别是用于预防和/或治疗选自（1）高血压的一种或多种病症，（2）心脏肥大和（3）心力衰竭。

9. 发明申请

US20050020695A1 Use of ERbeta-selective ligands for regulating fertility and compounds useful therefor 审中-公开
标题翻译：使用ERbeta选择性配体调节生育力和有用的化合物
公开(公告)号：US20050020695A1
公开(公告)日：2005-01-27
申请号：US10909540
申请日：2004-08-03
申请人： Christa Hegele-Hartung , Karl-Heinrich Fritzemeier , Hiroshi Yamanouchi , Olaf Peters , Dirk Kosemund , Gerd Mueller , Ingo Tornus , Gerd Schubert , Sven Ring
发明人： Christa Hegele-Hartung , Karl-Heinrich Fritzemeier , Hiroshi Yamanouchi , Olaf Peters , Dirk Kosemund , Gerd Mueller , Ingo Tornus , Gerd Schubert , Sven Ring
IPC分类号： A61K31/00 , A61K31/05 , A61K31/122 , A61K45/06 , A61K31/075 , C07C39/12
CPC分类号： A61K45/06 , A61K31/00 , A61K31/05 , A61K31/122
摘要： The present invention discloses the use of ERβ-selective ligands for production of medicaments for regulating fertility without additional use of a progestin. ERβ-agonists are used for treatment of infertility and ERβ-antagonists for contraception.
摘要翻译：本发明公开了ERbeta选择性配体用于生产用于调节生育力而不需要额外使用孕激素的药物。 ERbeta激动剂用于治疗不育症和ERbeta拮抗剂用于避孕。

10. 发明授权

US06794409B2 Use of ER&bgr;-selective ligands for regulating fertility and compounds useful therefor 失效
标题翻译：使用ERbeta选择性配体调节生育力和有用的化合物
公开(公告)号：US06794409B2
公开(公告)日：2004-09-21
申请号：US10083685
申请日：2002-02-27
申请人： Christa Hegele-Hartung , Karl-Heinrich Fritzemeier , Hiroshi Yamanouchi , Olaf Peters , Dirk Kosemund , Gerd Mueller , Ingo Tornus , Gerd Schubert , Sven Ring
发明人： Christa Hegele-Hartung , Karl-Heinrich Fritzemeier , Hiroshi Yamanouchi , Olaf Peters , Dirk Kosemund , Gerd Mueller , Ingo Tornus , Gerd Schubert , Sven Ring
IPC分类号： A61K31215
CPC分类号： A61K45/06 , A61K31/00 , A61K31/05 , A61K31/122
摘要： The present invention discloses the use of ER&bgr;-selective ligands for production of medicaments for regulating fertility without additional use of a progestin. ER&bgr;-agonists are used for treatment of infertility and ER&bgr;-antagonists for contraception.
摘要翻译：本发明公开了ERbeta选择性配体用于生产用于调节生育力的药物的用途，而不需要额外使用孕激素.Ebeta激动剂用于治疗不育症和用于避孕的ERbeta拮抗剂。

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